An inhibitor of DYRK1A

Leucettine L41 – 5 mg

Brand:
Cayman
CAS:
1112978-84-3
Storage:
-20
UN-No:
Non-Hazardous - /

Leucettine L41 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively).{53108} It also inhibits GSK3α/β and Pim1 with IC50 values of 0.41 and 4.1 µM, respectively. It inhibits phosphorylation of the serine/arginine (SR) protein 9G8 by DYRK2, DYRK3, CLK1, CLK2, and CLK4 and inhibits TNF-α-induced SRp75 and SRp55 phosphorylation in human microvascular endothelial cells when used at concentrations ranging from 0.1 to 10 µM. Leucettine L41 modulates alternative pre-RNA splicing of a synthetic CLK1 minigene in a reporter model. It prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by amyloid-β 25-35 (Item No. 24155) in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity.{53109} Leucettine L41 (0.4, 1.2, and 4 µg, i.c.v.) also prevents memory deficits induced by amyloid-β 25-35 in the same model.  

 

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SKU: 29225 - 5 mg Category:

Description

An inhibitor of DYRK1A, DYRK2, CLK1, and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively); an inhibitor of GSK3α/β and Pim1 (IC50s = 0.41and 4.1 µM, respectively); inhibits TNF-α-induced SRp75 and SRp55 phosphorylation in human microvascular endothelial cells at 0.1-10 µM; modulates alternative pre-RNA splicing of a synthetic CLK1 minigene; prevents amyloid-β 25-35-induced lipid peroxidation and ROS accumulation in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity; prevents amyloid-β 25-35-induced memory deficits in the same model at 0.4, 1.2, and 4 µg

Formal name: (5Z)-5-(1,3-benzodioxol-5-ylmethylene)-3,5-dihydro-2-(phenylamino)-4H-imidazol-4-one

Synonyms: 

Molecular weight: 307.3

CAS: 1112978-84-3

Purity: ≥98%

Formulation: A solid

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